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    Methods and composition of extended delivery of water insoluble drugs
    1.
    发明授权
    Methods and composition of extended delivery of water insoluble drugs 有权
    延长交付水不溶性药物的方法和组成

    公开(公告)号：US08535716B2

    公开(公告)日：2013-09-17

    申请号：US11097487

    申请日：2005-04-01

    Applicant: John Hilfinger ,  Jae Seung Kim ,  Paul Kijek

    Inventor： John Hilfinger ,  Jae Seung Kim ,  Paul Kijek

    IPC: A61K9/22

    CPC classification number: A61K9/2013 ,  A61K9/2081 ,  A61K9/2846 ,  A61K9/5015 ,  A61K9/5057 ,  A61K31/225

    Abstract: A pharmaceutical composition is provided that includes an active ingredient in the form of a powder or granule, a water soluble high molecular weight excipient and a water insoluble hydrophilic amphiphilic excipient. These ingredients are solution mixed and dried to form a modified pharmaceutical ingredient in simultaneous contact with both the water soluble high molecular weight excipient and the water insoluble hydrophilic amphiphilic excipient. Adjuvants are compacted about the modified pharmaceutical ingredient as well as a release control agent. The release control agent being present at levels from 1 to 40 total weight percent of the pharmaceutical composition.

    Abstract translation: 提供了药物组合物，其包含粉末或颗粒形式的活性成分，水溶性高分子量赋形剂和水不溶性亲水两亲性赋形剂。 这些成分是溶液混合并干燥以形成与水溶性高分子量赋形剂和水不溶性亲水性亲水性赋形剂同时接触的改性药物成分。 佐剂关于改性药物成分以及释放控制剂压实。 释放控制剂以药物组合物的总重量的1至40的水平存在。

    Prodrugs of Neuraminidase Inhibitors
    4.
    发明申请
    Prodrugs of Neuraminidase Inhibitors 有权
    神经氨酸酶抑制剂的前药

    公开(公告)号：US20140155350A1

    公开(公告)日：2014-06-05

    申请号：US14091004

    申请日：2013-11-26

    Applicant: John Hilfinger ,  Gordon Amidon

    Inventor： John Hilfinger ,  Gordon Amidon

    IPC: C07F7/12 ,  C07C279/16 ,  C07D307/89 ,  C07D231/14 ,  C07D309/28

    CPC classification number: C07F7/12 ,  A61K31/155 ,  A61K31/167 ,  A61K31/351 ,  C07C279/16 ,  C07D231/14 ,  C07D307/89 ,  C07D309/28

    Abstract: A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.

    Abstract translation: 提供了一类新的神经酰胺酶抑制剂前药，其特征在于被修饰以形成羰基乙氧基氨基酸的羧基的前药部分，羰基乙氧基二肽或羰基乙氧基三肽，修饰形成羰基乙氧基氨基酸的胍基， 羰基乙氧基二肽，羰基乙氧基三肽; 改性以形成未改变的治疗剂的酯化单一氨基酸，二肽或三肽的三乙胺的伯醇。 如此修饰以形成前药的示例性治疗剂包括扎那韦咪，奥司他韦和帕拉莫韦。 前药相对于未改变的神经氨酸酶抑制剂具有增加的口服生物利用度，并且在病毒繁殖周期中有效抑制涉及神经氨酸酶的病毒感染。

    Prodrugs of Neuraminidase Inhibitors
    5.
    发明申请
    Prodrugs of Neuraminidase Inhibitors 审中-公开
    神经氨酸酶抑制剂的前药

    公开(公告)号：US20120058937A9

    公开(公告)日：2012-03-08

    申请号：US12937624

    申请日：2009-04-15

    Applicant: John Hilfinger ,  Gordon Amidon

    Inventor： John Hilfinger ,  Gordon Amidon

    IPC: A61K38/06 ,  C07C229/48 ,  C07K5/08 ,  A61P31/16 ,  A61K31/351 ,  A61K31/215 ,  A61P31/12 ,  C07D309/28 ,  A61K38/05

    CPC classification number: C07F7/12 ,  A61K31/155 ,  A61K31/167 ,  A61K31/351 ,  C07C279/16 ,  C07D231/14 ,  C07D307/89 ,  C07D309/28

    Abstract: A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.

    Abstract translation: 提供了一类新的神经酰胺酶抑制剂前药，其特征在于被修饰以形成羰基乙氧基氨基酸的羧基的前药部分，羰基乙氧基二肽或羰基乙氧基三肽，修饰形成羰基乙氧基氨基酸的胍基， 羰基乙氧基二肽，羰基乙氧基三肽; 改性以形成未改变的治疗剂的酯化单一氨基酸，二肽或三肽的三乙胺的伯醇。 如此修饰以形成前药的示例性治疗剂包括扎那韦咪，奥司他韦和帕拉莫韦。 前药相对于未改变的神经氨酸酶抑制剂具有增加的口服生物利用度，并且在病毒繁殖周期中有效抑制涉及神经氨酸酶的病毒感染。

    Methods and compositions of gene delivery agents for systemic and local therapy
    6.
    发明申请
    Methods and compositions of gene delivery agents for systemic and local therapy 审中-公开
    用于全身和局部治疗的基因递送剂的方法和组成

    公开(公告)号：US20050026859A1

    公开(公告)日：2005-02-03

    申请号：US10706738

    申请日：2003-11-12

    Applicant: John Hilfinger ,  Brake Roessler ,  Phillip Kish

    Inventor： John Hilfinger ,  Brake Roessler ,  Phillip Kish

    IPC: A61K31/56 ,  A61K47/48 ,  A61K48/00 ,  A61K9/127 ,  C12N15/88

    CPC classification number: A61K31/56 ,  A61K47/554 ,  A61K47/645 ,  A61K48/00

    Abstract: A method is provided for the packaging of a nucleic acid with a chelating agent having a coordinating moiety linked to a central hydrophobic moiety that terminates in a hydrophilic moiety. The complex is well suited for oral and other forms of therapeutic administration of nucleic acids in order to exact systemic and/or localized gene delivery therapy. Intestinal epithelial cells, as well as non-epithelial cells within the gastrointestinal tract and other target cells, are transformed for short or long-term therapies through oral administration, direct injection, or infusive administrations. A nucleic acid conjugating agent particulate composition amenable for administration as a gene therapy composition is provided. The composition is readily adjusted to create a particle having a controlled size and net-zero, -positive, or -negative charge.

    Abstract translation: 提供了一种用于将核酸与螯合剂包装的方法，所述螯合剂具有与终止于亲水部分的中心疏水部分连接的配位部分。 该复合物非常适用于核酸的口服和其他形式的治疗性给药以便精确的全身和/或定位的基因递送疗法。 肠上皮细胞以及胃肠道和其他靶细胞内的非上皮细胞通过口服给药，直接注射或侵入性给药转化为短期或长期疗法。 提供了适于作为基因治疗组合物给药的核酸缀合剂颗粒组合物。 容易地调整组合物以产生具有受控尺寸和净零 - 正 - 或 - 负电荷的颗粒。

    Prodrugs of Neuraminidase Inhibitors
    8.
    发明申请
    Prodrugs of Neuraminidase Inhibitors 审中-公开
    神经氨酸酶抑制剂的前药

    公开(公告)号：US20110160127A1

    公开(公告)日：2011-06-30

    申请号：US12937624

    申请日：2009-04-15

    Applicant: John Hilfinger ,  Gordon Amidon

    Inventor： John Hilfinger ,  Gordon Amidon

    IPC: A61K38/06 ,  C07D309/28 ,  C07C229/48 ,  C07K5/08 ,  A61K38/05 ,  A61K31/351 ,  A61K31/215 ,  A61P31/12 ,  A61P31/16

    CPC classification number: C07F7/12 ,  A61K31/155 ,  A61K31/167 ,  A61K31/351 ,  C07C279/16 ,  C07D231/14 ,  C07D307/89 ,  C07D309/28

    Abstract: A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.

    Abstract translation: 提供了一类新的神经酰胺酶抑制剂前药，其特征在于被修饰以形成羰基乙氧基氨基酸的羧基的前药部分，羰基乙氧基二肽或羰基乙氧基三肽，修饰形成羰基乙氧基氨基酸的胍基， 羰基乙氧基二肽，羰基乙氧基三肽; 改性以形成未改变的治疗剂的酯化单一氨基酸，二肽或三肽的三乙胺的伯醇。 如此修饰以形成前药的示例性治疗剂包括扎那韦咪，奥司他韦和帕拉莫韦。 前药相对于未改变的神经氨酸酶抑制剂具有增加的口服生物利用度，并且在病毒繁殖周期中有效抑制涉及神经氨酸酶的病毒感染。

    PRODRUG COMPOSITION
    10.
    发明申请
    PRODRUG COMPOSITION 审中-公开
    PRODRUG组合物

    公开(公告)号：US20070167353A1

    公开(公告)日：2007-07-19

    申请号：US11690528

    申请日：2007-03-23

    Applicant: John Hilfinger ,  Wei Shen

    Inventor： John Hilfinger ,  Wei Shen

    IPC: A61K38/14 ,  A61K31/7076 ,  C07H19/16 ,  C07K9/00

    CPC classification number: C07K9/001 ,  A61K31/7076 ,  A61K38/14 ,  A61K45/06 ,  A61K47/542 ,  A61K47/555 ,  A61K47/65 ,  C07H19/16

    Abstract: A prodrug composition is provided which includes a pharmaceutical species and an amino acid having a covalent bond to the pharmaceutical species. A particular pharmaceutical species is adenosine arabinoside, also known as Ara A and by the trade name vidarabine. Ara A prodrugs of the present invention have increased bioavailability compared to the parent compound Ara A. The inventive prodrug is transported from the gastrointestinal lumen by a specific transporter and is enzymatically cleaved to yield Ara A, such that Ara A is delivered to the individual.

    Abstract translation: 提供了前药组合物，其包含药物物质和与药物物质具有共价键的氨基酸。 特定的药物种类是阿糖胞苷，也称为Ara A，商品名为阿糖腺苷。 本发明的Ara与母体化合物Ara A相比，本发明的前药具有增加的生物利用度。本发明的前药由特异性转运蛋白从胃肠腔输送，并被酶切割以产生Ara A，从而将Ara A递送至个体。

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